Method for preparing key intermediate of medication for anti AIDS
An anti-AIDS and intermediate technology, applied in the preparation of carboxylate/lactone, organic chemistry, etc., can solve the problems of large amount of three wastes, low total yield, etc. The effect of high purity
Inactive Publication Date: 2009-01-07
ZHEJIANG JIUZHOU PHARM CO LTD
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This method is feasible, but the amount of three wastes to be treated is relatively large, and the total yield is as low as about 35%.
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[0030] The following examples are used to further illustrate the present invention, but not to limit the scope of the present invention.
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This invention discloses a method for manufacturing the intermediate of an anti-AIDS drug. The method uses phenyl aldehyde as the raw material, and subjects it to condensation, reduction, Grignard reaction and hydrolysis to obtain (R)-3-hydroxyl-3-(20phenylethyl)-hexanoic acid. The yield is 50-60%.
Description
technical field [0001] The invention belongs to the technical field of chemical industry and pharmacy, and relates to a preparation method of a key intermediate (R)-3-hydroxyl-3-(2-phenylethyl)-hexanoic acid formula (2) compound of anti-HIV drug TIPRANAVIR. Background technique [0002] TIPRANAVIR, a compound of formula (1), is an HIV-1 protease inhibitor. [0003] [0004] (R)-3-Hydroxy-3-(2-phenylethyl)-hexanoic acid, the compound of formula (2), is the key intermediate of TIPRANAVIR. [0005] [0006] The synthetic method of (R)-3-hydroxyl-3-(2-phenylethyl)-hexanoic acid disclosed in the prior art mainly contains the following types: [0007] Described in J.Org.Chem.1998 63,7348-7356 is a starting material with 3-phenylhexanone, then reacts with the lithium salt of ethyl acetate to prepare the 3-hydroxyl-3-( 2-Phenylethyl)-hexanoic acid. (R)-3-Hydroxy-3-(2-phenylethyl)-hexanoic acid was obtained by resolution with (-)norephedrine. According to this method, lithi...
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IPC IPC(8): C07C59/50C07C51/09
Inventor 李文泽张达徐明东梅义将
Owner ZHEJIANG JIUZHOU PHARM CO LTD
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